CA3078654A1 - Inhibiteurs de tyrosine kinases mutantes de la famille des egfr - Google Patents
Inhibiteurs de tyrosine kinases mutantes de la famille des egfr Download PDFInfo
- Publication number
- CA3078654A1 CA3078654A1 CA3078654A CA3078654A CA3078654A1 CA 3078654 A1 CA3078654 A1 CA 3078654A1 CA 3078654 A CA3078654 A CA 3078654A CA 3078654 A CA3078654 A CA 3078654A CA 3078654 A1 CA3078654 A1 CA 3078654A1
- Authority
- CA
- Canada
- Prior art keywords
- alkyl
- tyrosine kinase
- cycloalkyl
- kinase inhibitor
- family tyrosine
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- 108060006698 EGF receptor Proteins 0.000 title claims abstract description 135
- 239000003112 inhibitor Substances 0.000 title description 26
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 title description 16
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 title description 16
- 102000001301 EGF receptor Human genes 0.000 claims abstract description 134
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims abstract description 59
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims abstract description 58
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims abstract description 47
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims abstract description 44
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims abstract description 44
- 230000035772 mutation Effects 0.000 claims abstract description 39
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- 150000001875 compounds Chemical class 0.000 claims description 88
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- 239000001257 hydrogen Substances 0.000 claims description 69
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 69
- 125000003118 aryl group Chemical group 0.000 claims description 52
- 229910052736 halogen Inorganic materials 0.000 claims description 35
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- 150000002367 halogens Chemical group 0.000 claims description 32
- 125000001072 heteroaryl group Chemical group 0.000 claims description 32
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/027—Organoboranes and organoborohydrides
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
L'invention concerne un inhibiteur de tyrosine kinase de la famille des récepteurs du facteur de croissance épidermique (EGFR) comprenant un groupe fonctionnel qui peut se lier au résidu sérine S797 dans l'EGFR portant une mutation C797S ou au résidu sérine S805 dans le HER2 portant une mutation C805S.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US201762574110P | 2017-10-18 | 2017-10-18 | |
US62/574,110 | 2017-10-18 | ||
PCT/US2018/056516 WO2019079599A1 (fr) | 2017-10-18 | 2018-10-18 | Inhibiteurs de tyrosine kinases mutantes de la famille des egfr |
Publications (1)
Publication Number | Publication Date |
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CA3078654A1 true CA3078654A1 (fr) | 2019-04-25 |
Family
ID=66174232
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CA3078654A Pending CA3078654A1 (fr) | 2017-10-18 | 2018-10-18 | Inhibiteurs de tyrosine kinases mutantes de la famille des egfr |
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US (2) | US20200261455A1 (fr) |
EP (1) | EP3697416A4 (fr) |
JP (1) | JP2021500350A (fr) |
KR (1) | KR20200072498A (fr) |
CN (1) | CN111542322A (fr) |
AR (1) | AR113451A1 (fr) |
AU (1) | AU2018353142A1 (fr) |
BR (1) | BR112020007783A2 (fr) |
CA (1) | CA3078654A1 (fr) |
IL (1) | IL274015A (fr) |
MX (1) | MX2020004036A (fr) |
PH (1) | PH12020550259A1 (fr) |
RU (1) | RU2020117315A (fr) |
SG (1) | SG11202003307XA (fr) |
TW (1) | TW201922726A (fr) |
UY (1) | UY37935A (fr) |
WO (1) | WO2019079599A1 (fr) |
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JP2022501344A (ja) * | 2018-09-21 | 2022-01-06 | スペクトラム ファーマシューティカルズ インコーポレイテッド | 新規キナゾリンegfr阻害剤 |
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GB0207323D0 (en) * | 2002-03-28 | 2002-05-08 | Astrazeneca Ab | Compounds |
TWI324597B (en) * | 2002-03-28 | 2010-05-11 | Astrazeneca Ab | Quinazoline derivatives |
GB0321620D0 (en) * | 2003-09-16 | 2003-10-15 | Astrazeneca Ab | Quinazoline derivatives |
CA2539022A1 (fr) * | 2003-09-16 | 2005-03-24 | Astrazeneca Ab | Derives de quinozaline en tant qu'inhibiteurs de la tyrosine kinase |
TWI377944B (en) * | 2007-06-05 | 2012-12-01 | Hanmi Holdings Co Ltd | Novel amide derivative for inhibiting the growth of cancer cells |
KR101705158B1 (ko) * | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Egfr 억제제 및 질환 치료방법 |
US9034885B2 (en) * | 2012-01-13 | 2015-05-19 | Acea Biosciences Inc. | EGFR modulators and uses thereof |
CN104761544B (zh) * | 2014-01-03 | 2019-03-15 | 北京轩义医药科技有限公司 | Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂 |
AU2015277786B2 (en) * | 2014-06-19 | 2019-04-18 | Takeda Pharmaceutical Company Limited | Heteroaryl compounds for kinase inhibition |
KR102327053B1 (ko) * | 2017-03-16 | 2021-11-17 | 기초과학연구원 | 퀴나졸린, 퀴놀린 유도체 및 egfr 키나제 억제제로서의 용도 |
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2018
- 2018-10-17 AR ARP180103010A patent/AR113451A1/es unknown
- 2018-10-17 UY UY0001037935A patent/UY37935A/es not_active Application Discontinuation
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2022
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JP2021500350A (ja) | 2021-01-07 |
US20230106731A1 (en) | 2023-04-06 |
MX2020004036A (es) | 2021-01-15 |
EP3697416A4 (fr) | 2021-06-02 |
RU2020117315A (ru) | 2021-11-17 |
TW201922726A (zh) | 2019-06-16 |
US20200261455A1 (en) | 2020-08-20 |
BR112020007783A2 (pt) | 2020-10-20 |
CN111542322A (zh) | 2020-08-14 |
UY37935A (es) | 2020-03-31 |
RU2020117315A3 (fr) | 2022-04-25 |
KR20200072498A (ko) | 2020-06-22 |
EP3697416A1 (fr) | 2020-08-26 |
AR113451A1 (es) | 2020-05-06 |
IL274015A (en) | 2020-06-30 |
AU2018353142A1 (en) | 2020-05-07 |
WO2019079599A8 (fr) | 2020-06-25 |
WO2019079599A1 (fr) | 2019-04-25 |
PH12020550259A1 (en) | 2021-03-01 |
SG11202003307XA (en) | 2020-05-28 |
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